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Several dehidropregnenolone derivatives functionalized at C
2024-03-04
Several 16-dehidropregnenolone derivatives functionalized at C3, C4, C5 and C6 (Fig. 7) were prepared and evaluated as 5α-reductase inhibitors bearing in mind that after the formation of an enzyme-steroid complex a nucleophilic portion of the enzyme attacks the double bond of the steroid through Mic
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br Results br Discussion Although they do not have
2024-03-04
Results Discussion Although they do not have protein-coding capacity, lncRNAs make up a large part of the transcripts of the genome, and they play fundamental roles in carcinogenesis and osteosarcoma progression through regulation of tumor proliferation and metastasis. These lncRNAs include MA
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The enzyme Arginase ARG plays a role in the hepatic
2024-03-04
The enzyme Arginase 1 (ARG1) plays a role in the hepatic urea cycle by hydrolyzing L-arginine to L-ornithine and urea [13]. In the context of macrophages and MDSCs, ARG1 expression redirects L-arginine metabolism to abolish cytotoxic nitric oxide production [14], suppress T-cell function [15], [16],
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The Limitations of our data include the absence
2024-03-04
The Limitations of our data include the absence of functional/behavioral assessments and lack of direct comparison with females which would require additional studies and conceivably support sex-specific interventions for stroke [50]. Competing interests Acknowledgements This study was suppor
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Coumarin Given that neither case is
2024-03-04
Given that neither case is derived from multiplex Coumarin with affected individuals, principles of Mendelian segregation cannot be applied to implicate the T201S mutation in causing familial CJD. In addition, like many rare gene variants, it is not possible to apply practice guidelines such as the
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br Under normal physiological conditions the agonist binds
2024-03-02
Under normal physiological conditions, the agonist binds to AT1R on the surface of the plasma membrane and activates the receptor, mediating downstream signaling. Then, activated AT1R is phosphorylated by protein kinase C (PKC) [13] or G protein coupled receptor kinases (GPKs, such as GRK2 [13], G
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br Angiotensin receptor neprilysin inhibitors Sacubitril val
2024-03-02
Angiotensin receptor-neprilysin inhibitors Sacubitril/valsartan is the first-in-class ARNI, comprising of molecular moieties of valsartan (ARB) and a neprilysin inhibitor prodrug, sacubitril (AHU377) [51]. Upon ingestion, sacubitril is rapidly metabolised into an active neprilysin inhibitor, sacu
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Amyloid fibrils are insoluble high molecular weight
2024-03-02
Amyloid fibrils are insoluble, high-molecular-weight, non-crystalline aggregates and traditional experimental techniques for structure determination such as X-ray and solution NMR cannot resolve their high resolution structures [64], [68]. However, amyloid fibrils exhibit various advantageous featur
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The advantage of active immunotherapy is long term
2024-03-02
The advantage of active immunotherapy is long-term antibody production from short-term drug administration at limited cost. Conversely, immune response may be inconsistent or lacking, especially in older individuals, and adverse reactions—if immunologically based—may also be long-lasting. Initial ex
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Regarding the HT B receptors they act as terminal
2024-03-02
Regarding the 5-HT1B receptors, they act as terminal receptors and are involved in the presynaptic regulation of the release of 5-HT. But at spinal level these receptors are principally situated post-synaptically (Sari, 2004). The ability of autoreceptors to regulate extracellular levels of 5-HT dur
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br Perspectives and challenges Previously the main focus of
2024-03-02
Perspectives and challenges Previously, the main focus of development of adenosine targets for pain was on A1Rs, due to prominent antinociception in multiple preclinical models and preliminary observations in human trials. However, delivery of agonists can be limited by other (e.g. cardiovascular
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Both subcutaneous s c and
2024-03-02
Both subcutaneous (s.c.) and mucosal administration of short synthetic peptide derivatives of AChR prevent the onset of EAMG, but do not treat ongoing EAMG [80], [81], [82], [83], [84], [85]. The selection of peptides for treatment is mainly based on the identification of immunodominant T- and B-cel
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Finasteride was the first steroidal
2024-03-02
Finasteride (13) was the first steroidal 5α-reductase inhibitor approved by the US Food and Drug Administration (FDA) in 1992 for treatment of BPH. In fact, long term clinical studies with this drug demonstrated a sustained reduction of the prostatic specific antigen and an overall improvement in BH
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Inactivation of autophagy can also impact
2024-03-02
Inactivation of autophagy can also impact the surface internalization of MHC I molecules, leading to increased antigen presentation. Inactivation of autophagy factors Atg5 and Atg7 in DCs causes elevation of MHC I surface levels by decreasing endocytosis due to a poor recruitment of adaptor-associat
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According to the present observations the
2024-03-01
According to the present observations, the Ampkα1 isoform promotes AP-1 transcriptional activity and thereby fosters Axitinib of AP-1 target genes in cardiomyocytes via activation of Pkcζ. The transcription factor AP-1 plays a decisive role during cardiac remodeling [24], [25], [26], [37]. AP-1 mod
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